Design, synthesis and evaluation of unnatural peptides as T1R2/T1R3 PAMs.,Bioorganic & Medicinal Chemistry Letters

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Design, synthesis and evaluation of unnatural peptides as T1R2/T1R3 PAMs.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-01-27 , DOI: 10.1016/j.bmcl.2020.127000
Kei Yamada ₁ , Ryo Matsumoto ₁ , Yumiko Suzuki ₁ , Suguru Mori ₁ , Seiji Kitajima ₁

Affiliation

The sweet receptor T1R2/T1R3 is a member of G protein-coupled receptor family and recognizes diverse natural and synthetic sweeteners. Previously, we reported a novel class of positive allosteric modulators (PAMs) of T1R2/T1R3 comprising an unnatural tripeptide structure. We classified the structure of these PAMs into three parts: "head", "linker" and "tail". Here, we report the design, synthesis and evaluation of various tail structures to obtain highly active unnatural peptide structure of PAM. In conclusion, we discovered the novel unnatural tetrapeptide with highly potent PAM activity on T1R2/T1R3 in a cell-based assay system.

中文翻译：

设计，合成和评估非天然肽T1R2 / T1R3 PAM。

甜味受体T1R2 / T1R3是G蛋白偶联受体家族的成员，可识别多种天然和合成甜味剂。以前，我们报道了T1R2 / T1R3的一类新颖的正构构调节剂（PAM），其中包括非天然的三肽结构。我们将这些PAM的结构分为三个部分：“头”，“链接器”和“尾部”。在这里，我们报告各种尾巴结构的设计，合成和评估，以获得高活性的PAM非天然肽结构。总之，我们在基于细胞的测定系统中发现了对T1R2 / T1R3具有高度有效PAM活性的新型非天然四肽。

更新日期：2020-01-27

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